Olumacostat glasaretil Acetyl-CoA carboxylase (ACC) inhibitor Acne therapy

被引:1
|
作者
Baroudi, B. [1 ]
Shealy, E. R. [1 ]
Cardwell, C. A. [1 ]
Alinia, H. [1 ]
Feldman, S. R. [1 ,2 ,3 ]
机构
[1] Wake Forest Sch Med, Ctr Dermatol Res, Dept Dermatol, Winston Salem, NC 27157 USA
[2] Wake Forest Sch Med, Dept Pathol, Winston Salem, NC 27157 USA
[3] Wake Forest Sch Med, Dept Social Sci & Hlth Policy, Winston Salem, NC 27157 USA
关键词
Olumacostat glasaretil; Acne; Papules; Pustules; Topical; Androgenic; Acetyl-CoA carboxylase (ACC) inhibitor; BENZOYL PEROXIDE; VULGARIS; MANAGEMENT; RESISTANCE; COENZYME;
D O I
10.1358/dof.2018.043.03.2766398
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Acne vulgaris is a common dermatologic condition affecting adolescents and adults. Systemic and topical therapies have been developed to target different mechanisms in the pathogenesis of acne. Olumacostat glasaretil (OG) is a novel topical agent that targets sebum production in the treatment of acne vulgaris. OG's active metabolite acts as a competitive inhibitor of the rate-limiting enzyme of fatty acid synthesis, acetylcoenzyme A (CoA) carboxylase (ACC). ACC catalyzes malonylCoA formation and sebum production. OG is efficacious in the treatment of acne vulgaris and has a low side effect profile. Phase IIa and IIb trials note side effects including applicationsite erythema and dryness, and nasopharyngitis. Phase III trials are currently underway. The new mechanism of action of OG is sensible, attractive and exciting, but the available data do not demonstrate that it provides a quantum leap forward over existing therapies.
引用
收藏
页码:175 / 179
页数:5
相关论文
共 50 条
  • [41] STUDY OF ACETYL-COA CARBOXYLASE IN MAIZE GERM
    AHUJA, KL
    SUKHIJA, PS
    BHATIA, IS
    INDIAN JOURNAL OF BIOCHEMISTRY & BIOPHYSICS, 1979, 16 (01): : 76 - 76
  • [42] Acetyl-CoA Carboxylase Herbicide Tolerance in Bermudagrass
    Grimshaw, Austin L.
    Schwartz, Brian M.
    Grey, Timothy L.
    McCullough, Patrick E.
    Raymer, Paul L.
    Webster, Theodore M.
    Kowalewski, A. R.
    Tate, Trent M.
    Parrott, Wayne A.
    AGRONOMY JOURNAL, 2014, 106 (03) : 925 - 930
  • [43] DETERMINATION OF THE DOMAIN ORGANIZATION OF ACETYL-COA CARBOXYLASE
    MABROUK, GM
    HUANG, WY
    STOOPS, JK
    WAKIL, SJ
    FEDERATION PROCEEDINGS, 1986, 45 (06) : 1532 - 1532
  • [44] INACTIVATION OF ACETYL-COA CARBOXYLASE BY COLD TREATMENT
    LANDMAN, AD
    INTERNATIONAL JOURNAL OF BIOCHEMISTRY, 1976, 7 (6-7): : 313 - 315
  • [45] Acetyl-CoA carboxylase - A graminicide target site
    Herbert, D
    Walker, KA
    Price, LJ
    Cole, DJ
    Pallett, KE
    Ridley, SM
    Harwood, JL
    PESTICIDE SCIENCE, 1997, 50 (01): : 67 - 71
  • [46] Regulation and structure of the heteromeric acetyl-CoA carboxylase
    Salie, Matthew J.
    Thelen, Jay J.
    BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS, 2016, 1861 (09): : 1207 - 1213
  • [47] Bimodal activation of acetyl-CoA carboxylase by glutamate
    Boone, AN
    Chan, A
    Kulpa, JE
    Brownsey, RW
    JOURNAL OF BIOLOGICAL CHEMISTRY, 2000, 275 (15) : 10819 - 10825
  • [48] COENZYME-A ACTIVATION OF ACETYL-COA CARBOXYLASE
    YEH, LA
    SONG, CS
    KIM, KH
    JOURNAL OF BIOLOGICAL CHEMISTRY, 1981, 256 (05) : 2289 - 2296
  • [49] Acetyl-CoA carboxylase activity in the oil palm
    Sambanthamurthi, R
    Ohlrogge, JB
    PHYSIOLOGY, BIOCHEMISTRY AND MOLECULAR BIOLOGY OF PLANT LIPIDS, 1997, : 26 - 28
  • [50] Piperazine Oxadiazole Inhibitors of Acetyl-CoA Carboxylase
    Bourbeau, Matthew P.
    Siegmund, Aaron
    Allen, John G.
    Shu, Hong
    Fotsch, Christopher
    Bartberger, Michael D.
    Kim, Ki-Won
    Komorowski, Renee
    Graham, Melissa
    Busby, James
    Wang, Minghan
    Meyer, James
    Xu, Yang
    Salyers, Kevin
    Fielden, Mark
    Veniant, Murielle M.
    Gu, Wei
    JOURNAL OF MEDICINAL CHEMISTRY, 2013, 56 (24) : 10132 - 10141